GSK'963

製品コードS8642 バッチS864201

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₄H₁₈N₂O

分子量

230.31

CAS No.

2049868-46-2

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

200 mg/mL (868.39 mM)

Ethanol

46 mg/mL (199.73 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	10.000mg/ml (43.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.
in vitro	GSK'963 inhibits RIP1-dependent cell death with an IC50 of between 1 and 4 nM in human and murine cells^[1].
in vivo	GSK'963 is a potent inhibitor of a TNF+zVAD-mediated lethal shock. At 2 mg/kg, this compound would maintain blood concentrations above the concentration required for 90% inhibition of RIP1 activity for an extended period of time compared with Nec-1^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	BMDM
	濃度	100 nM
	反応時間	30 min
	実験の流れ	For immunoblot analysis, BMDM pretreated with GSK'963 (100 nM), this compound (100 nM) or Nec-1 (10 μM) for 30 min, are stimulated with 50 ng/ml TNF for 5 and 15 min. Lysates prepared in 1× Cell Lysis Buffer containing protease and phosphatase inhibitors are separated on 4-12% SDS-PAGE and blotted onto nitrocellulose membrane. Blots are probed for IκB, phospho-IκB, and tubulin as a loading control.
動物実験	動物モデル	C57BL/6 mice
	投薬量	0.2, 2 and 10 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/27551444/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

RIPK1 is required for ZBP1-driven necroptosis in human cells [ PLoS Biol, 2025, 23(2):e3002845]	PubMed: 39982916
Bacillus cereus cereolysin O induces pyroptosis in an undecapeptide-dependent manner [ Cell Death Discov, 2024, 10(1):122]	PubMed: 38458999
Polyunsaturated fatty acids-induced ferroptosis suppresses pancreatic cancer growth [ Sci Rep, 2024, 14(1):4409]	PubMed: 38388563
RIPK1 is essential for Herpes Simplex Virus-triggered ZBP1-dependent necroptosis in human cells [ bioRxiv, 2024, 2024.09.17.613393]	PubMed: 39345610
Toxoplasma gondii secreted effectors co-opt host repressor complexes to inhibit necroptosis [ Cell Host Microbe, 2021, S1931-3128(21)00192-X]	PubMed: 34043960
The MK2/Hsp27 axis is a major survival mechanism for pancreatic ductal adenocarcinoma under genotoxic stress [ Sci Transl Med, 2021, 13(622):eabb5445]	PubMed: 34851698

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。